Characterisation of biotinylated liposomes for in vivo targeting applications

FEBS Letters

Acerbis, Giulia⁵  Loughrey, Helen C.²  Cannon, Ann-Marie²  Masserini, Massimo¹  Sudati, Francesco³  Soria, Marco R.⁵  Bottiroli, Giovanni⁴  Ferraretto, Anita⁵ 

[1] Department of Medical Biochemistry, University of Milan, Italy;Department of Biochemistry, University College Galway, Galway, Ireland;Department of Nuclear Medicine, HSR, Milan, Italy;Centro di Istiochemica del CNR, Pavia, Italy;DIBIT, HSR, Milan, Italy

关键词: Liposome;    Streptavidin;    Biotin;    Ganglioside;    Polyethyleneglycol;    Targeted liposome;    GM1;    monosialoganglioside;    PEG;    polyethyleneglycol;    biotin-DPPE;    JV-biotinoyl dipahnitoyl phosphatidyl-ethanolamine;    EPPS;    N-(2-hydroxyethyl) piperazme-N'-3-propanesulphonic acid;    HEPES;    N-(2-hydroxyethyl) piperazme-N'-2-ethanesulphonic acid;    DTPA;    di-ethylene-tetraamino pentaacetic acid;    HBS;    25 mM HEPES;    150 mM NaCl;    pH 7.5;    PBS;    phosphate buffered saline;   

DOI  :  10.1016/0014-5793(93)80509-S

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Liposomes containing monosialoganglioside (G_M1) or polyethylene glycol (PEG) lipid derivatives have prolonged circulation in the blood. This favours liposome extravasation to tumour sites. In this report it is shown that inclusion of G_M1, PEG₅₅₀-DPPE or PEG₂₀₀₀-DPFE in liposomes containing biotin-DPPE significantly diminished the ability of vesicles to bind to streptavidin in vitro. Steric inhibition due to the bulky head group of these lipids was least for biotin-DPPE liposomes containing G_M1. Biodistribution studies in C26 tumour-bearing mice showed that G_M1-liposomes containing small amounts of biotin-DPPE have long circulation life-times in the blood. Using fluorescent microscopic techniques, liposomes containing both G_M1 and biotin-DPPE were detected within extra-vascular spaces in tumours. In addition it was shown that biotin-DPPE in G_M1-liposomes bound streptavidin in situ. These results suggest that G_M1-liposomes containing biotin-DPPE have potential use as diagnostic or therapeutic reagents in pre-targeting applications dependent on the high-affinity interaction of biotin with streptavidin.

【 授权许可】

Unknown